Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src).
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 5 mg | 2-3 weeks | $ 674 | |
| 10 mg | 2-3 weeks | $ 1145 | |
| 20 mg | 2-3 weeks | $ 1819 | |
| 50 mg | 2-3 weeks | $ 3802 | |
| 100 mg | 2-3 weeks | $ 6007 |
| Description | Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src). |
| Targets&IC50 | PKCη:0.052 μM, PKCβ2:5.9 nM, PKCδ:0.25 μM, PKCγ:0.3 μM, PKCβ1:4.7 nM |
| In vitro | LY333531 strikingly decreases the chance of HUVEC survival and the effect of LY333531 on apoptotic cell death in HUVEC significantly increases compared with the AGEs group. Blockade of PKC-beta up-regulates the expression of Bax and Bad proteins and down-regulates the expression of Bcl-2 protein. Moreover, LY333531 reduces the ratio of Bcl-2/Bax. LY333531 can further prompt AGEs-induced endothelial cells apoptosis. The increased expression of Bax, Bad and decreased expression of Bcl-2 and Bcl-2/Bax ratio are associated with the apoptotic process. |
| In vivo | A significant up-regulation of TGF-b1, Smad2 and Smad3 mRNA expression was observed in diabetic rats, which was alleviated by administration of ruboxistaurin. |
| Synonyms | LY333531 HCl, LY 333531 hydrochloride, Ruboxistaurin |
| CAS No. | 169939-93-9 |
| Chemical Formula | C28H29ClN4O3 |
| Molecular Weight | 505.02 |
| Solubility | DMSO: 10.1 mg/mL (20 mM) |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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